Gemcitabine HCl

Alias: Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar
Cat No.:V1423 Purity: ≥98%
GemcitabineHCl (formerly also known as LY-188011, NSC-613327; dFdC; dFdCyd; trade name: Gemzar), the hydrochloride salt of gemcitabine which is anantimetabolite anticancer drug,is a potent DNA synthesis inhibitor approved for cancer treatment.
Gemcitabine HCl Chemical Structure CAS No.: 122111-03-9
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Gemcitabine HCl (formerly also known as LY-188011, NSC-613327; dFdC; dFdCyd; trade name: Gemzar), the hydrochloride salt of gemcitabine which is an antimetabolite anticancer drug, is a potent DNA synthesis inhibitor approved for cancer treatment. In PANC1, MIAPaCa2, BxPC3, and Capan2 cells, it inhibits DNA synthesis with IC50s of 50 nM, 40 nM, 18 nM, and 12 nM, respectively. Difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP) are the active metabolites of gemcitabine that are produced intracellularly. The deoxynucleotide pool available for DNA synthesis is reduced when dFdCDP inhibits ribonucleotide reductase.

Biological Activity I Assay Protocols (From Reference)
Targets
DNA synthesis (Capan2 cells) ( IC50 = 12 nM ); DNA synthesis (BxPC3 cells) ( IC50 = 18 nM ); DNA synthesis (MIAPaCa2 cells) ( IC50 = 40 nM ); DNA synthesis (PANC1 cells) ( IC50 = 50 nM )
ln Vitro

Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) is an effective and potent way to kill senescent cells in both humans and mice[4]. Gemcitabine Hydrochloride exhibits growth inhibition against BxPC-3, Mia Paca-2, PANC-1, PL-45, and AsPC-1 cells, with IC50 values of 37.6, 42.9, 92.7, 89.3, and 131.4 nM, in that order[1].

ln Vivo
Gemcitabine Hydrochloride can be supplied to rats via endotracheal spray once a week for nine weeks without causing noticeable toxicity, up to a maximum tolerated dose of 4 mg/kg. At doses of 2, 4, and 6 mg/kg, gemcitabine is less toxic when administered by lung than when taken orally[2].
The median survival time is increased by more than 30 days when compared to the placebo group in the LSL-KrasG12D/+, LSL-Trp53R172H, and Pdx-1-Cre mice treated with either gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine Hydrochloride[3].
Cell Assay
In a 96-well plate, BxPC-3, MIA PaCa-2, and PANC-1 cells are seeded. Cells are treated for a further 24 or 48 hours with vehicle, DMAPT, and/or Gemcitabine after 24 hours. Using the Cell Death Detection ELISA, apoptosis is measured in relation to vehicle-treated cells by counting the quantity of cytoplasmic histone-associated DNA fragments.
Animal Protocol
Dissolved in PBS; 50 or 100 mg/kg; i.p. injection
Athymic nude mice with MIA PaCa-2 cells
References

[1]. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80.

[2]. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206.

[3]. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149.

[4]. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H11F2N3O4.HCI
Molecular Weight
299.66
Exact Mass
299.05
Elemental Analysis
C, 36.07; H, 4.04; Cl, 11.83; F, 12.68; N, 14.02; O, 21.36
CAS #
122111-03-9
Appearance
White solid powder
SMILES
C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F.Cl
InChi Key
OKKDEIYWILRZIA-OSZBKLCCSA-N
InChi Code
InChI=1S/C9H11F2N3O4.ClH/c10-9(11)6(16)4(3-15)18-7(9)14-2-1-5(12)13-8(14)17;/h1-2,4,6-7,15-16H,3H2,(H2,12,13,17);1H/t4-,6-,7-;/m1./s1
Chemical Name
4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride
Synonyms
Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~19 mg/mL (~63.4 mM)
Ethanol: <1 mg/mL(slightly soluble or insoluble)
Solubility (In Vivo)
Saline: 20 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3371 mL 16.6856 mL 33.3712 mL
5 mM 0.6674 mL 3.3371 mL 6.6742 mL
10 mM 0.3337 mL 1.6686 mL 3.3371 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02769832 Active
Recruiting
Drug: Nab-paclitaxel
Drug: Gemcitabine
Small Cell Lung Cancer
(SCLC)
Muhammad Furqan August 29, 2016 Phase 2
NCT00479128 Active
Recruiting
Drug: Bortezomib
Drug: Gemcitabine
Solid Tumor
Urethral Cancer
M.D. Anderson Cancer Center September 28, 2006 Phase 1
NCT03520790 Active
Recruiting
Drug: Gemcitabine
Other: Placebo
Pancreatic Cancer Dana-Farber Cancer Institute December 5, 2018 Phase 1
Phase 2
NCT03558087 Active
Recruiting
Drug: Nivolumab
Drug: Gemcitabine
Bladder Cancer Matthew Galsky July 13, 2018 Phase 2
NCT03507491 Active
Recruiting
Drug: Gemcitabine
Drug: Nab-paclitaxel
Cancer Emory University August 27, 2018 Phase 1
Biological Data
  • Cytotoxicity of I3C and gemcitabine (GEM) at clinical relevant concentrations in hTERT-HPNE and BxPC-3 cells cells. Anticancer Res . 2011 Oct;31(10):3171-80.
  • Effect of I3C in combination with gemcitabine (GEM) on hENT1 protein expression in pancreatic cancer cell lines. Anticancer Res . 2011 Oct;31(10):3171-80.
  • Combined inhibition of hTrx1 and RRM1 produced a synergistic anticancer effect in cancer cells and xenograft mice. A, SW480 or SW620 cells were treated with the indicated concentrations of gemcitabine or PX-12 for 72 h, and cell viability was measured with Cell Counting Kit-8 assays. J Biol Chem . 2017 Jun 2;292(22):9136-9149.
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